Target intelligence / Profile preview

Dopamine receptors D1, D2, D3, and D4 (DRD1-DRD4)

Target
DRD1-DRD4
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

Dopamine receptors D1, D2, D3, and D4 are a subset of the G protein-coupled receptor (GPCR) family that mediate the physiological effects of the neurotransmitter dopamine in the central nervous system and peripheral tissues [2, 4]. This specific grouping is considered incomplete as it excludes the D5 receptor, which along with D1 constitutes the D1-like family, while D2, D3, and D4 form the D2-like family [2, 13]. These receptors play critical roles in regulating motor control, motivation, reward, and cognitive functions such as working memory and attention [3, 11]. Dysregulation of these receptors is central to the pathophysiology of several neuropsychiatric conditions, including schizophrenia, Parkinson's disease, and attention-deficit hyperactivity disorder (ADHD) [4, 5]. Pharmacological intervention often involves dopamine receptor antagonists for treating psychosis or agonists for managing motor symptoms in Parkinson's [10, 11]. However, targeting these receptors can lead to significant side effects, such as extrapyramidal symptoms or impulse control disorders, due to their widespread expression and diverse functional roles [11, 17].

Other names
Dopamine receptor D1Dopamine receptor D2Dopamine receptor D3Dopamine receptor D4DRD1DRD2DRD3DRD4D1-like dopamine receptorsD2-like dopamine receptors
02

Mechanism of action

Dopamine receptor antagonism, agonism, and partial agonism

03

Biological functions

Signal transductionMotor controlReward processingCognitive functionNeuromodulationExecutive functionRegulation of renal function
04

Disease associations

SchizophreniaParkinson's diseaseAttention-deficit hyperactivity disorderSubstance use disorderBipolar disorderDepressionTourette's syndrome
05

Safety considerations

Extrapyramidal symptomsTardive dyskinesiaHyperprolactinemiaMetabolic syndromeImpulse control disordersNeuroleptic malignant syndromeOrthostatic hypotension
06

Interacting drugs

Haloperidol

9 more in the full profile.

07

Biomarkers

PET imaging of dopamine receptor occupancySerum prolactin levelsPeripheral blood DRD3/DRD4 mRNA levelsStriatal dopamine transporter (DAT) imaging

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